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sacituzumab tirumotecan   Click here for help

GtoPdb Ligand ID: 13791

Synonyms: Jiataile® | MK-2870 | sac-TMT | SKB-264 | SKB264
Approved drug
sacituzumab tirumotecan is an approved drug
Compound class: Antibody
Comment: Sacituzumab tirumotecan (SKB264/MK-2870) is an antibody-drug conjugate (ADC) [1-2]. It is the same humanized anti-TROP-2 monoclonal antibody as the previously approved ADC sacituzumab govitecan, but carrying a different topoisomerase inhibitor payload (tirumotecan/KL610023) that is a belotecan-derivative. TROP-2 is a transmembrane glycoprotein, cell surface antigen which has oncogenic activity in cancers of epithelial origin [6], but expression is restricted in normal tissue. Directing the topoisomerase inhibitor selectively to cancer cells via TROP-2 binding is predicted to limit toxicity towards healthy tissue/cells.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
References
1. Cheng Y, Yuan X, Tian Q, Huang X, Chen Y, Pu Y, Long H, Xu M, Ji Y, Xie J et al.. (2022)
Preclinical profiles of SKB264, a novel anti-TROP2 antibody conjugated to topoisomerase inhibitor, demonstrated promising antitumor efficacy compared to IMMU-132.
Front Oncol, 12: 951589. [PMID:36620535]
2. Ettorre VM, Palmieri L, Santin AD. (2025)
Clinical pharmacologic considerations for antibody-drug conjugate in gynecologic cancers.
Expert Rev Clin Pharmacol, 18 (7): 461-469. [PMID:40660679]
3. Fang W, Li X, Wang Q, Meng X, Zheng W, Sun L, Yao W, Zhuang W, Fan Y, Zhuo M et al.. (2025)
Sacituzumab tirumotecan versus docetaxel for previously treated EGFR-mutated advanced non-small cell lung cancer: multicentre, open label, randomised controlled trial.
BMJ, 389: e085680. [PMID:40473437]
4. Hong S, Wang Q, Cheng Y, Luo Y, Qu X, Zhu H, Ding Z, Li X, Wu L, Wang Y et al.. (2025)
First-line sacituzumab tirumotecan with tagitanlimab in advanced non-small-cell lung cancer: a phase 2 trial.
Nat Med, 31 (11): 3654-3661. [PMID:40830660]
5. Ouyang Q, Rodon J, Liang Y, Wu X, Li Q, Song L, Yan M, Tong Z, Liu Y, Wainberg ZA et al.. (2025)
Results of a phase 1/2 study of sacituzumab tirumotecan in patients with unresectable locally advanced or metastatic solid tumors refractory to standard therapies.
J Hematol Oncol, 18 (1): 61. [PMID:40481574]
6. Stoyanova T, Goldstein AS, Cai H, Drake JM, Huang J, Witte ON. (2012)
Regulated proteolysis of Trop2 drives epithelial hyperplasia and stem cell self-renewal via β-catenin signaling.
Genes Dev, 26 (20): 2271-85. [PMID:23070813]
7. Yin Y, Fan Y, Ouyang Q, Song L, Wang X, Li W, Li M, Yan X, Wang S, Sun T et al.. (2025)
Sacituzumab tirumotecan in previously treated metastatic triple-negative breast cancer: a randomized phase 3 trial.
Nat Med, 31 (6): 1969-1975. [PMID:40217078]